Steroidal esters of 17-oximino-5 androsten-3β-ol were synthesized from dehydroandrosterone acetate. These compounds were tested for their antiproliferating activity and 5α-Reductase inhibitory activity in comparison to finasteride. Decreased androgen levels have been found in serum of animals treated with newly synthesized compounds. These compounds have shown better cytotoxicity as comparison to the clinically used drug finasteride. Therefore these compounds can be useful in the treatment of androgen dependent disorders of prostate alone or by synergistic effect they can decrease the size of prostate due to their antiproliferating activity. The compound TRB-263 was synthesized from the diosgenin involving marker degradation, oximation, Beckmann rearrangement, acid hydrolysis, oximation and esterification. Analytical method for the synthesized compound (TRB-263) was developed using RP-HPLC. Octyldecylsilane column was selected and a rapid, sensitive HPLC method for determination of TRB-263 was optimized and validated. Optimized chromatographic conditions were achieved after a series of screening experiments with elution systems of acidified Phosphate Buffer-ACN, in various proportions. It was found that ACN and phosphate buffer of pH 3.0 gave better peaks than other mobile phase composition. Optimized chromatographic conditions consist of mobile phase Acetonitrile (ACN): Phosphate buffer (PBS) pH 3.0 in the ratio of 16:20 (%v/v). Retention time was found to be 3.9 min. for TRB-263 at flow rate of 1.0 mL/min. Bioanalytical method was developed in human plasma for simultaneous estimation of TRB-263 by RP-HPLC with UV detection at 236nm. The chromatographic conditions employed for bioanalytical method development were exactly the same as that of analytical method. For the bioanalytical method, Acetonitrile was used as a protein precipitant and the ratio of plasma: ACN (0.2: 1.8mL) was used for the extraction.
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